[EN] SUBSTITUTED 4,5,6,7-TETRAHYDRO-PYRAZOLO[1,5-a]PYRAZINE DERIVATIVES AND 5,6,7,8-TETRAHYDRO-4H-PYRAZOLO[1,5-a][1,4]DIAZEPINE DERIVATIVES AS ROS1 INHIBITORS<br/>[FR] DÉRIVÉS 4,5,6,7-TÉTRAHYDRO-PYRAZOLO[1,5-A]PYRAZINE SUBSTITUÉS ET DÉRIVÉS 5,6,7,8-TÉTRAHYDRO-4H-PYRAZOLO[1,5-A][1,4]DIAZÉPINE UTILISÉS COMME INHIBITEURS DE ROS1
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2015144799A1
公开(公告)日:2015-10-01
The present invention relates to substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-a]pyrazine derivatives and 5,6,7,8-tetrahydro-4H-pyrazolo[1,5-a][1,4]diazepine derivatives of formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as ROS 1 inhibitors. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
P–alkene bidentate ligands: an unusual ligand effect in Pd-catalysed Suzuki reactions
作者:D. Bradley G. Williams、Megan L. Shaw
DOI:10.1016/j.tet.2006.12.012
日期:2007.2
ehyde was used to prepare a variety of electronically and sterically varied ligands using Wittig or aldol methodology in high yields. Pd-catalysed Suzuki reactions were evaluated using these ligands. The influence of the functional group on the alkene, which is in direct conjugation with the phosphorus centre of the ligand, was visible in the activity profiles of the reactions. In general, the activity
Olefin metathesis catalyst bearing a chelating phosphine ligand
作者:Christina Lexer、Daniel Burtscher、Bernhard Perner、Eyal Tzur、N. Gabriel Lemcoff、Christian Slugovc
DOI:10.1016/j.jorganchem.2011.03.005
日期:2011.6
for the complex (SPY-5-34)-dichloro-(κ2(C,P)-diphenyl-(2-benzylidene)-phosphine)-(1,3-bis(2,4,6-trimethylphenyl)-4,5-dihydro-imidazol-2-ylidene)-ruthenium (2) was elaborated and the title compound was tested as latent initiator in Ring Opening Metathesis Polymerization (ROMP) and as catalyst for Ring-Closing Metathesis (RCM) at elevated temperatures. While not particularly suited as latent initiator
Deprotonation of η<sup>2</sup>(4e)-bonded alkynes as a pathway to σ,η<sup>2</sup>(3e)-prop-2-ynyl, η<sup>5</sup>-pentadienyl and η<sup>4</sup>-trans-1,3-diene substituted molybdenum complexes
作者:Carla Carfagna、Robert J. Deeth、Michael Green、Mary F. Mahon、Jacqueline M. Mclnnes、Sylvan Pellegrini、Christopher B. Woolhouse
DOI:10.1039/dt9950003975
日期:——
Li[N(SiMe3)2] to the halogenobis(alkyne) complexes [MoBr(η2-MeC2R)2(η-C5H5)](R = Me or Ph) resulted in a dehydrohalogenation reaction and formation of the σ,η2(3e)-prop-2-ynyl/η2(4e)-alkyne-substituted complexes [Moσ,η2(3e)-CH2C2R}η2(4e)-MeC2R}(η-C5H5)](R = Ph 7 or Me). The structure when R = Ph has been confirmed by a single-crystal X-ray diffraction study. The η2(4e)-bondedalkyne and σ,η2(3e)-prop-2-ynyl
的Li [N(森达的另外3)2 ]将halogenobis(炔)络合物[MoBr(η 2 -MeC 2 R)2(η-C 5 H ^ 5)](R = Me或PH)导致了脱卤化氢反应和形成的σ,η 2(3E) -丙-2-炔基/η 2(4E)-alkyne取代配合物[沫σ,η 2(3E)-CH 2 C ^ 2 R} η 2(4E )-MeC 2 R}(η-C 5 H ^ 5)](R =苯基7或Me)。通过单晶X射线衍射研究已经证实了当R = Ph时的结构。该η 2(4E)键合的炔和σ,η 2(3E) -丙-2-炔基配体位于平面基本上平行于所述η-C的5 ħ 5配位体,具有C(1)-C(2) - C(3)角和Mo–C(1),Mo–C(2)和Mo–C(3)的丙-2-炔基片段的键长为146.1(6)°,2.278(6),2.164( 5)和2.105(5)Å。所述M-σ,η的性质2 -C 3 H ^
Five‐ and Six‐Membered Cobaltocycles with C,P‐Chelating Ligands through Regiospecific Cyclometalation of Mono(2‐Substituted) Triphenylphosphane
P)}tris(trimethylphosphane)cobalt] (4). The molecular structure shows a trigonal-bipyramidal configuration of the cobalt atom accommodating a six-membered metallacycle. 2-(Diphenylphosphanyl)styrene replaces two trimethylphosphaneligands to give [2-(diphenylphosphanyl)styrene-(C,C-η2,P)}methylbis(trimethylphosphane)cobalt] (5), avoiding metalation. Replacement of equatorial trimethylphosphane in compounds